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Assay Detail

CHEMBL1769765

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Inhibition of CYP2D6
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Procopiou PA, Browning C, Buckley JM, Clark KL, Fechner L, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Kranz M, Looker BE, Morriss KM, Parton DL, Russell LJ, Slack RJ, Sollis SL, Vile S, Watts CJ.
J Med Chem (2011) 54 : 2183 -2195
PubMed 21381763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.70 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1767164 GSK-1004723 2.0 1 7.40
CHEMBL639 AZELASTINE 4.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1767164 GSK-1004723 IC50 = 40.0 nM 7.40
CHEMBL639 AZELASTINE IC50 = 1000.0 nM 6.00